Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers

William C. Drewe; Stephen Neidle

doi:10.1039/B814576H

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Chemical Communications

Issue 42, 2008

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Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers

William C. Drewe and Stephen Neidle

Chem. Commun., 2008, 5295-5297

DOI: 10.1039/B814576H
Received 21 Aug 2008, Accepted 22 Sep 2008
First published on the web 30 Sep 2008

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Abstract
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A series of diarylurea ligands were designed to interact selectively with G-quadruplexes and were synthesised using copper(I) catalysed ‘click’ chemistry to incorporate the 1,4-substituted 1,2,3-triazole ring into the core of the ligands; the optimal ligands demonstrate a high degree of selective telomeric G-quadruplex stabilisation and are not cytotoxic in several cancer cell lines.

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Experimental procedures for synthesis, FRET and cell culture;HPLC purity; FRET melting curves
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Chemical Communications

Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers

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